Quiz 5 Phar 605

lisinopril with hydrochlorothiazide

antihypertensive

a number of different actions, most related to suppression of the renin-angiotensin-aldosterone system. Competitively inhibits angiotensin-converting enzyme (ACE) to decrease synthesis of angiotensin II, one of the most potent vasoconstrictors known. Then this leads to decrease release of aldosterone, that then decreases sodium and water reabsorption and lowers plasma volume. Also involved with degradation of bradykinin, a vasodilator. Hydrochlorothiazide inhibits the reabsorption of sodium and chloride at the distal renal tubule.

Tablets

lisinopril with hydrochlorothiazide

antihypertensive

a number of different actions, most related to suppression of the renin-angiotensin-aldosterone system. Competitively inhibits angiotensin-converting enzyme (ACE) to decrease synthesis of angiotensin II, one of the most potent vasoconstrictors known. Then this leads to decrease release of aldosterone, that then decreases sodium and water reabsorption and lowers plasma volume. Also involved with degradation of bradykinin, a vasodilator. Hydrochlorothiazide inhibits the reabsorption of sodium and chloride at the distal renal tubule.

Tablets

Fenofibrate (nanocrystallized)

antihyperlipidemic

lowers Total-C, LDL-C, and triglycerides by activation of peroxisome proliferator activated receptor-a (PPARa). Through this mechanism, fenofibrate increases lipolysis and elimination of triglyceride-rich particles from plasma by activating lipoprotein lipase and reducing production of apoprotein C-III. A decrease in triglycerides results in a change in the composition of LDL to larger particles which are catabolized rapidly. Also reducing serum uric acid levels in hyperuricemic and normal individuals by increasing urinary excretion of uric acid.

Tablets (nanocrystallized)

ziprasidone hydrochloride

antipsychotic

exact mechanism unknown. Thought to act by antagonism of dopamine D2 and serotonin 5HT2 receptors. Also shown to be an antagonist at histamine H2 and alpha-1-adrenergic receptors.

• Capsules
• Injection
• Suspension

olmesartan medoxomil

antihypertensive

Angiotensin II is a potent vasoconstrictor, the primary vasoactive hormone of the renin-angiotensin system and an important component in the pathophysiology of hypertension. It also stimulates aldosterone secretion by the adrenal cortex. Olmesartan medoxomil is a prodrug which is hydrolyzed to olmesartan during absoprtion from the GI tract. Olmesartan blocks the vasoconstrictor and aldosterone-secreting effects of antiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor found in many tissues. Olmesartan does not inhibit ACE, nor does it bind to or block other hormone receptors or ion channels known to the be important in cardiovascular regulation.

Tablets

thyroid, dessicated

hormone/thyroid

exact mechanism unknown. Thought to be due to protein synthesis control, resulting in: (1) a regulation of growth and development, (2) an increase in metabolic rate, (3) inhibition of the secretion of thyrotropin by the pituitary, and 94) various effects on lipid and carbohydrate metabolism.

Tablets

aripiprazole

antipsychotic

exact mechanism unknown. May be due to a combination of partial agonist activity at dopamine D2 and serotonin 5-HT1A receptors and antagonist activity at 5-HT2A receptors. Metabolized by CYP3A4 and CYP2D6 enzymes to dehydro-aripipazole following oral administration and has some activity at the D2 receptors and represents 40% of the parent drug exposure in plasma.

• Tablets (regular, ODT)
• Oral solution
• Injection

ranitidine hydrochloride

gastric antisecretory

competitively and reversibly inhibits histamine at the H2 receptors, including receptors on gastric cells. H2 antagonists are highly selective, they do not affect H1 receptors and do not affect acetylcholine. Ranitidine inhibits fasting and nocturnal secretions, secretions stimulated by food, caffeine, and insulin, and secretions casued by histimine, gastrin, and muscarinic agonists.

• Tablets (regular, EFFERdose)
• Syrup (peppermint flavor)
• Injection

oxycodone hydrochloride

opioid analgesic

analgesia produced centrally via action on the central opiate receptors. Other therapeutic effects of oxycodone include anxiolysis, euphoria, and feelings of relaxation. Respiratory depression occurs via direct action on brain stem respiratory centers. Depression of the cough reflex occurs via direct action on the cough center in the medulla. Oxycodone causes a reduction in motility associated with an increase in smooth muscle tone in the antrum of the stomach and duodenum.

• Tablets
• Solution
• Concentrate

ramipril

antihypertensive

thought to be due to its suppression of the renin-angiotensin-aldosterone system by competitively inhibiting the angiotensin-converting enzyme (ACE). ACE converts angiotensin I to angiotensin II, one of the most potent vasoconstrictors known. Inhibition of ACE decreases plasma angiotensin II which leads to decreased aldosterone secretion. The latter may cause an increase in serum potassium. The net result is a decrease in peripheral arterial resistance.

Capsules

clopidogrel bisulfate

hematological agent

inhibits platelet aggregation by irreversibly modifying platelet receptors thereby selectively inhibiting the binding of adenosine diphosphate (ADP) to the receptor. This results in an inhibition of the ADP-mediated activation of the glycoprotein GPIIb/IIIa complex and an inhibition of platelet aggregation.

Tablets

ezetimibe

antihyperlipidemic

a class of lipid-lowering compounds that selectively inhibits the intestinal absorption of cholesterol and related phytosterols. It appears to act at the brush border of the small intestine to inhibit cholesterol absorption thereby decreasing the delivery of cholesterol to the liver. After oral administration, ezetimibe is absorbed and extensively conjugated to a pharmacologically active phenolic glucuronide.

Tablets

spironolactone

diuretic

competitive antagonism of aldosterone, primarily at the aldosterone-dependent Na+/K+ exchange sites in the distal convoluted renal tubule.

Tablets

tiotropium bromide (inhalation)

antiasthmatic

a long-acting antagonist of the action of acetylcholine at the M3-receptors in the smooth muscle of the bronchial tree. This antagonism results in bronchodilation which lasts for greater than 24 hours. Chemically, tiotropium is a synthetic, non-chiral, quaternary ammonium compound.

Inhalation powder

famotidine

gastric antisecretory

competitively inhibits histamine at the H2 receptors, including receptors on gastric cells. This inhibition is reversible. Both the acid concentration and volume of gastric secretion are suppressed. Changes in pepsin secretion are proportional to volume output. Inhibits basal, nocturnal, and food stimulated gastric secretion.

• Tablets
• Powder for oral suspension (cherry-banana-mint flavor)
• Premixed injection
• Injection

codeine phosphate with guaifenesin

antitussive/expectorant

Guaifenesin promotes lower respiratory tract drainage by thinning bronchial secretions, lubricating irritated respiratory tract membranes through increased mucous flow, and facilitating removal of viscous, inspissated mucous. Codeine depresses the cough reflex center in the medulla oblongota.

Syrup

codeine phosphate with guaifenesin

antitussive/expectorant

Guaifenesin promotes lower respiratory tract drainage by thinning bronchial secretions, lubricating irritated respiratory tract membranes through increased mucous flow, and facilitating removal of viscous, inspissated mucous. Codeine depresses the cough reflex center in the medulla oblongota.

syrup

norgestimate and/with ethinyl estradiol

oral contraceptive

suppression of luteinizing hormone (LH) and follicle stimulation hormone (FSH) result in the inhibition of ovulation. Thickening of the cervical mucous (inhibiting sperm penetration) and alteration of the endometrium (which inhibits implantation) may also contribute to their effectiveness.

• Tablets
• 28 day Dialpaks (7 green inert tablets)

norgestimate and/with ethinyl estradiol

oral contraceptive

suppression of luteinizing hormone (LH) and follicle stimulation hormone (FSH) result in the inhibition of ovulation. Thickening of the cervical mucous (inhibiting sperm penetration) and alteration of the endometrium (which inhibits implantation) may also contribute to their effectiveness.

• Tablets
• 28 day Dialpaks (7 green inert tablets)

norgestimate and/with ethinyl estradiol

oral contraceptive

suppression of luteinizing hormone (LH) and follicle stimulation hormone (FSH) result in the inhibition of ovulation. Thickening of the cervical mucous (inhibiting sperm penetration) and alteration of the endometrium (which inhibits implantation) may also contribute to their effectiveness.

• Tablets
• 28 day Dialpaks (7 green inert tablets)

ibuprofen

nonsteroidal anti-inflammatory

produces a reversible inhibition of cyclooxygenase which results in a decreased synthesis of prostaglandins. Prostaglandins sensitize pain receptors resulting in a lower pain threshold. By inhibiting their production, ibuprofen raises the pain threshold so fewer pain impulses reach the CNS. Prostaglandins are involved in setting the normal set point in the thermoregulatory center of the hypothalamus. By inhibiting their production, ibuprofen resets the normal set point and increases heat loss from the body through increased cutaneous blood flow and sweating. Prostaglandins are also involved in vasodilation and plasma exudate formation at inflammation sites. Again inhibiting their production, ibuprofen can decrease inflammation.

• Tablets
• nonprescription - liquid, chewable (for children)

memantine hydrochloride

agent for Alzheimer's Dementia

Persistant activation of central nervous system N-methyl-D-aspartate (NMDA) receptors by the excitatory amino acid glutamate has been hypothesized to contribute to the symptomatology of Alzheimer's disease. Memantine is thought to exert its therapeutic effect through its action as a low to moderate affinity uncompetitive (open-channel) NMDA receptor antagonist. It binds perferentially to the NMDA receptor-operated cation channels. It shows little to no affinity for GABA, benzodiazepine, dopamine, adrenergic, histamine, and glycine receptors or for voltage-dependent Ca2+, Na+, or K+ channels. It does show antagonistic effects at the 5HT3 receptor and a slight inhibition of nicotinic acetylcholine receptors.

• Tablets
• Oral solution (alcohol-free, sugar-free)

memantine hydrochloride

agent for Alzheimer's Dementia

Persistant activation of central nervous system N-methyl-D-aspartate (NMDA) receptors by the excitatory amino acid glutamate has been hypothesized to contribute to the symptomatology of Alzheimer's disease. Memantine is thought to exert its therapeutic effect through its action as a low to moderate affinity uncompetitive (open-channel) NMDA receptor antagonist. It binds perferentially to the NMDA receptor-operated cation channels. It shows little to no affinity for GABA, benzodiazepine, dopamine, adrenergic, histamine, and glycine receptors or for voltage-dependent Ca2+, Na+, or K+ channels. It does show antagonistic effects at the 5HT3 receptor and a slight inhibition of nicotinic acetylcholine receptors.

Capsules (EXTENDED)

folic acid

vitamin

an important vitamin required for the synthesis of thymidylate, synthesis of purine nucleotides, and for maintenance of normal erythropoiesis. A deficiency of folic acid can result from inadequate dietary intake, from diseases of the small intestine, and from diseases of the liver which interfere with the recirculation of folate through enterohepatic cycle. Folic acid deficiency can lead to megaloblastic anemias in adults and children and in neural tube defects in unborn infants.

• Tablets (OTC, Rx)
• Injection

folic acid

vitamin

an important vitamin required for the synthesis of thymidylate, synthesis of purine nucleotides, and for maintenance of normal erythropoiesis. A deficiency of folic acid can result from inadequate dietary intake, from diseases of the small intestine, and from diseases of the liver which interfere with the recirculation of folate through enterohepatic cycle. Folic acid deficiency can lead to megaloblastic anemias in adults and children and in neural tube defects in unborn infants.

• Tablets (OTC, Rx)
• Injection

folic acid

vitamin

an important vitamin required for the synthesis of thymidylate, synthesis of purine nucleotides, and for maintenance of normal erythropoiesis. A deficiency of folic acid can result from inadequate dietary intake, from diseases of the small intestine, and from diseases of the liver which interfere with the recirculation of folate through enterohepatic cycle. Folic acid deficiency can lead to megaloblastic anemias in adults and children and in neural tube defects in unborn infants.

• Tablets (OTC, Rx)
• Injection

folic acid

vitamin

an important vitamin required for the synthesis of thymidylate, synthesis of purine nucleotides, and for maintenance of normal erythropoiesis. A deficiency of folic acid can result from inadequate dietary intake, from diseases of the small intestine, and from diseases of the liver which interfere with the recirculation of folate through enterohepatic cycle. Folic acid deficiency can lead to megaloblastic anemias in adults and children and in neural tube defects in unborn infants.

• Tablets (OTC, Rx)
• Injection

cephalexin monohydrate

cephalosporin antibiotic

first generation cephalosporin which inhibits bacterial cell wall synthesis via acylationof the transpeptidase enzyme. This acylation occurs in the third and final stage of bacterial cell wall synthesis and is believed to be due to the structural similarity of the cephalosporin nucleus to D-alanyl-D-alanine.

• Tablets
• Capsules
• Powder for oral suspension